Cell penetrating peptides functionalized gambogic acid-nanostructured lipid carrier for cancer treatment
Tumor-targeted delivery is considered a crucial component of current anticancer drug development and is the best approach to increase the efficacy and reduce the toxicity. Nanomedicine, particularly ligand-based nanoparticles have shown a great potential for active targeting of tumor. Cell penetrati...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2018-01-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/10717544.2018.1446474 |
| _version_ | 1828472873175482368 |
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| author | Rui Huang Jiawei Li Dereje Kebebe Yumei Wu Bing Zhang Zhidong Liu |
| author_facet | Rui Huang Jiawei Li Dereje Kebebe Yumei Wu Bing Zhang Zhidong Liu |
| author_sort | Rui Huang |
| collection | DOAJ |
| description | Tumor-targeted delivery is considered a crucial component of current anticancer drug development and is the best approach to increase the efficacy and reduce the toxicity. Nanomedicine, particularly ligand-based nanoparticles have shown a great potential for active targeting of tumor. Cell penetrating peptide is one of the promising ligands in a targeted cancer therapy. In this study, the gambogic acid-loaded nanostructured lipid carrier (GA-NLC) was modified with two kinds of cell penetrating peptides (cRGD and RGERPPR). The GA-NLC was prepared by emulsification and solvent evaporation method and coupled with cRGD, RGERPPR, and combination cRGD and RGERPPR to form GA-NLC-cRGD, GA-NLC-RGE, and GA-NLC-cRGD/RGE, respectively. The formulations were characterized by their particle size and morphology, zeta potential, encapsulation efficiency, and differential scanning calorimetry. In vitro cytotoxicity and cellular uptake study of the formulations were performed against breast cancer cell (MDA-MB-231). Furthermore, in vivo biodistribution and antitumor activity of the formulations were determined by in vivo imaging and in tumor-bearing nude mice, respectively. The result of in vitro cytotoxicity study showed that GA-NLC-RGE exhibited a significantly higher cytotoxicity on MDA-MB-231 as compared with GA-NLC and GA-Sol. Similarly, RGE-Cou-6-NLC showed remarkably higher uptake by the cells than other NLCs over the incubation period. The in vivo imaging study has demonstrated that among the formulations, the RGE-decorated DiR-NLC were more accumulated in the tumor site. The in vivo antitumor activity revealed that RGE-GA-NLC inhibits the tumor growth more efficiently than other formulations. In conclusion, RGERPPR has a potential as an effective carrier in targeting drug delivery of anticancer agents. |
| first_indexed | 2024-12-11T05:36:13Z |
| format | Article |
| id | doaj.art-6664a3aff7bf416295f1548bfcd2b6d7 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-11T05:36:13Z |
| publishDate | 2018-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-6664a3aff7bf416295f1548bfcd2b6d72022-12-22T01:19:16ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642018-01-0125175776510.1080/10717544.2018.14464741446474Cell penetrating peptides functionalized gambogic acid-nanostructured lipid carrier for cancer treatmentRui Huang0Jiawei Li1Dereje Kebebe2Yumei Wu3Bing Zhang4Zhidong Liu5Tianjin University of Traditional Chinese MedicineTianjin University of Traditional Chinese MedicineTianjin University of Traditional Chinese MedicineTianjin University of Traditional Chinese MedicineTianjin University of Traditional Chinese MedicineTianjin University of Traditional Chinese MedicineTumor-targeted delivery is considered a crucial component of current anticancer drug development and is the best approach to increase the efficacy and reduce the toxicity. Nanomedicine, particularly ligand-based nanoparticles have shown a great potential for active targeting of tumor. Cell penetrating peptide is one of the promising ligands in a targeted cancer therapy. In this study, the gambogic acid-loaded nanostructured lipid carrier (GA-NLC) was modified with two kinds of cell penetrating peptides (cRGD and RGERPPR). The GA-NLC was prepared by emulsification and solvent evaporation method and coupled with cRGD, RGERPPR, and combination cRGD and RGERPPR to form GA-NLC-cRGD, GA-NLC-RGE, and GA-NLC-cRGD/RGE, respectively. The formulations were characterized by their particle size and morphology, zeta potential, encapsulation efficiency, and differential scanning calorimetry. In vitro cytotoxicity and cellular uptake study of the formulations were performed against breast cancer cell (MDA-MB-231). Furthermore, in vivo biodistribution and antitumor activity of the formulations were determined by in vivo imaging and in tumor-bearing nude mice, respectively. The result of in vitro cytotoxicity study showed that GA-NLC-RGE exhibited a significantly higher cytotoxicity on MDA-MB-231 as compared with GA-NLC and GA-Sol. Similarly, RGE-Cou-6-NLC showed remarkably higher uptake by the cells than other NLCs over the incubation period. The in vivo imaging study has demonstrated that among the formulations, the RGE-decorated DiR-NLC were more accumulated in the tumor site. The in vivo antitumor activity revealed that RGE-GA-NLC inhibits the tumor growth more efficiently than other formulations. In conclusion, RGERPPR has a potential as an effective carrier in targeting drug delivery of anticancer agents.http://dx.doi.org/10.1080/10717544.2018.1446474cancercell penetrating peptidenanostructured lipid carriertumor targetinggambogic acid |
| spellingShingle | Rui Huang Jiawei Li Dereje Kebebe Yumei Wu Bing Zhang Zhidong Liu Cell penetrating peptides functionalized gambogic acid-nanostructured lipid carrier for cancer treatment Drug Delivery cancer cell penetrating peptide nanostructured lipid carrier tumor targeting gambogic acid |
| title | Cell penetrating peptides functionalized gambogic acid-nanostructured lipid carrier for cancer treatment |
| title_full | Cell penetrating peptides functionalized gambogic acid-nanostructured lipid carrier for cancer treatment |
| title_fullStr | Cell penetrating peptides functionalized gambogic acid-nanostructured lipid carrier for cancer treatment |
| title_full_unstemmed | Cell penetrating peptides functionalized gambogic acid-nanostructured lipid carrier for cancer treatment |
| title_short | Cell penetrating peptides functionalized gambogic acid-nanostructured lipid carrier for cancer treatment |
| title_sort | cell penetrating peptides functionalized gambogic acid nanostructured lipid carrier for cancer treatment |
| topic | cancer cell penetrating peptide nanostructured lipid carrier tumor targeting gambogic acid |
| url | http://dx.doi.org/10.1080/10717544.2018.1446474 |
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